biostudies-literatureAlvaro BSInstituto de Salud Carlos IIIConselleria de Cultura, Educación y Ciencia, Generalitat Valencianae202500904https://www.ebi.ac.uk/biostudies/studies/S-EPMC12860552biostudies-literatureUnknown21(2)Cancer caused 9.9 million deaths in 2020, and natural products and/or their structural analogs represent the greatest number of approved small-molecules antitumor agents. Benzopyran and quinoline heterocycles have demonstrated cytotoxic activity against different cancer cell lines. Due to its high therapeutic potential, we report the synthesis of 2-propanamide- and 2-propanamine-dihydrobenzopyrans bearing different amine moieties in the side chain, as well as the 7-carbon prenylated derivatives (analogous to natural polyalthidin). Next, we synthesized the 2-substituted and 2,3-disubstituted quinolines as benzopyran analogs. We evaluated the cytotoxic activity of all nitrogenated derivatives against human cancer cell lines, including A549 (lung cancer), A2058 (melanoma), HepG2 (hepatocellulChemMedChemSynthesis of Benzopyrans and Quinolines with Nitrogenated Chain and Their Cytotoxicity Against Human Cancer Cell Lines.PMC12860552Grant AICO/2021/081Grant PI21/02045Alvaro BSVillarroel-Vicente CGarcia ARamos MCMackenzie TACortes DVila LTormo JRCabedo NfalseSynthesis of Benzopyrans and Quinolines with Nitrogenated Chain and Their Cytotoxicity Against Human Cancer Cell Lines.Cancer caused 9.9 million deaths in 2020, and natural products and/or their structural analogs represent the greatest number of approved small-molecules antitumor agents. Benzopyran and quinoline heterocycles have demonstrated cytotoxic activity against different cancer cell lines. Due to its high therapeutic potential, we report the synthesis of 2-propanamide- and 2-propanamine-dihydrobenzopyrans bearing different amine moieties in the side chain, as well as the 7-carbon prenylated derivatives (analogous to natural polyalthidin). Next, we synthesized the 2-substituted and 2,3-disubstituted quinolines as benzopyran analogs. We evaluated the cytotoxic activity of all nitrogenated derivatives against human cancer cell lines, including A549 (lung cancer), A2058 (melanoma), HepG2 (hepatocellul2026-01-01T00:00:00Z2026 Jan2026-06-15T06:30:32.046Z2026-06-15T03:08:46.11ZS-EPMC128605524161930610.1002/cmdc.202500904